Synthesis and antiviral activity of some novel indole-2-carboxylate derivatives

A series of novel indole-2-carboxylate derivatives were synthesized and assayed to determine their in vitro broad-spectrum antiviral activities. The biological results showed that some of the synthesized compounds exhibited potent broad-spectrum antiviral activity. Notably, compound 8f showed the hi...

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Detalles Bibliográficos
Autores principales: Xue, Situ, Ma, Linlin, Gao, Rongmei, Li, Yuhuan, Li, Zhuorong
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2014
Materias:
Original Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4629079/
https://www.ncbi.nlm.nih.gov/pubmed/26579401
http://dx.doi.org/10.1016/j.apsb.2014.06.003
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author Xue, Situ
Ma, Linlin
Gao, Rongmei
Li, Yuhuan
Li, Zhuorong
author_facet Xue, Situ
Ma, Linlin
Gao, Rongmei
Li, Yuhuan
Li, Zhuorong
author_sort Xue, Situ
collection PubMed
description A series of novel indole-2-carboxylate derivatives were synthesized and assayed to determine their in vitro broad-spectrum antiviral activities. The biological results showed that some of the synthesized compounds exhibited potent broad-spectrum antiviral activity. Notably, compound 8f showed the highest SI value (17.1) to Cox B3 virus. Compound 14f showed both potent inhibitory activity against influenza A (IC(50)=7.53 μmol/L) and the highest SI value (12.1). SAR results showed that the alkyloxy at the 4-position of indole ring was not crucial to the antiviral activities. Incorporation of an acetyl substituent at the amino group disfavored antiviral activity towards RNA viruses.
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spelling pubmed-46290792015-11-17 Synthesis and antiviral activity of some novel indole-2-carboxylate derivatives Xue, Situ Ma, Linlin Gao, Rongmei Li, Yuhuan Li, Zhuorong Acta Pharm Sin B Original Article A series of novel indole-2-carboxylate derivatives were synthesized and assayed to determine their in vitro broad-spectrum antiviral activities. The biological results showed that some of the synthesized compounds exhibited potent broad-spectrum antiviral activity. Notably, compound 8f showed the highest SI value (17.1) to Cox B3 virus. Compound 14f showed both potent inhibitory activity against influenza A (IC(50)=7.53 μmol/L) and the highest SI value (12.1). SAR results showed that the alkyloxy at the 4-position of indole ring was not crucial to the antiviral activities. Incorporation of an acetyl substituent at the amino group disfavored antiviral activity towards RNA viruses. Elsevier 2014-08 2014-07-16 /pmc/articles/PMC4629079/ /pubmed/26579401 http://dx.doi.org/10.1016/j.apsb.2014.06.003 Text en © 2014 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V. http://creativecommons.org/licenses/by-nc-nd/3.0/ This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/3.0/).
spellingShingle Original Article
Xue, Situ
Ma, Linlin
Gao, Rongmei
Li, Yuhuan
Li, Zhuorong
Synthesis and antiviral activity of some novel indole-2-carboxylate derivatives
title Synthesis and antiviral activity of some novel indole-2-carboxylate derivatives
title_full Synthesis and antiviral activity of some novel indole-2-carboxylate derivatives
title_fullStr Synthesis and antiviral activity of some novel indole-2-carboxylate derivatives
title_full_unstemmed Synthesis and antiviral activity of some novel indole-2-carboxylate derivatives
title_short Synthesis and antiviral activity of some novel indole-2-carboxylate derivatives
title_sort synthesis and antiviral activity of some novel indole-2-carboxylate derivatives
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4629079/
https://www.ncbi.nlm.nih.gov/pubmed/26579401
http://dx.doi.org/10.1016/j.apsb.2014.06.003
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AT gaorongmei synthesisandantiviralactivityofsomenovelindole2carboxylatederivatives
AT liyuhuan synthesisandantiviralactivityofsomenovelindole2carboxylatederivatives
AT lizhuorong synthesisandantiviralactivityofsomenovelindole2carboxylatederivatives

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